Novel Zinc(II) Complexes of Heterocyclic Ligands as Antimicrobial Agents: Synthesis, Characterisation, and Antimicrobial Studies

The synthesis and antimicrobial activity of novel Zn(II) metal complexes derived from three novel heterocyclic Schiff base ligands 8-[(Z)-{[3-(N-methylamino)propyl]imino}methyl]-7-hydroxy-4-methyl-2H-chromen-2-one, 2-[(E)-{[4-(1H-1,2,4-triazol-1-ylmethyl)phenyl]imino}methyl]phenol, and (4S)-4-{4-[(E)-(2-hydroxybenzylidene)amino]benzyl}-1,3-oxazolidin-2-one have been described. These Schiff base ligands and metal complexes are characterised by spectroscopic techniques. According to these data, we propose an octahedral geometry to all the metal complexes. Antimicrobial activity of the Schiff base ligand and its metal complexes was studied against Gram negative bacteria: E. coli and Pseudomonas fluorescens, Gram positive bacteria: Staphylococcus aureus, and also against fungi, that is, C. albicans and A. niger. Some of the metal complexes show significant antifungal activity (MIC < 0.2 μg/mL). The “in vitro” data has identified [Zn(NMAPIMHMC)2]·2H2O, [Zn(TMPIMP)2]·2H2O, and [Zn(HBABO)2]·2H2O as potential therapeutic antifungal agents against C. albicans and A. niger

A review on quinoline hydrazone derivatives as a new class of potent antitubercular and anticancer agents

Tuberculosis (TB) and Cancer remains a global public health problem in recent years. There is an urgent need for the screening of new bioactive molecules with new targets and with a different mechanism of action. Among heterocyclic compounds, compounds with Quinoline core gained much importance in medicinal chemistry. Quinoline hydrazone scaffold plays an important role in anti-tuberculosis and anticancer drug development as their derivatives have shown outstanding results. This broad spectrum of biological and biochemical activities has been further assisted by the synthetic flexibility of quinoline, which permits the invention of a large number of structurally varied hydrazone derivatives and their metal complexes. In order to pave the way for future advanced research, there is a need to collect and analyze the latest information available so far in this promising area. In this review, we have compiled and discussed the published reports specifically on anti-tuberculosis and anticancer potential of quinoline hydrazone derivatives. It is hoped that this review will be helpful for researchers in developing a new view in the search for rational designs of more active and less toxic quinoline-based anti-TB and anticancer drugs. Keywords: Biological activity, Quinoline, Hydrazone, Cancer, Tuberculosi

SYNTHESIS OF DIAZO COMPOUNDS FROM AMINO BENZOPYRANO THIAZOLES

ABSTRACT 8-Amino-6-chlorocoumarine (5) has been synthesized by multistep synthesis (by known literature methods) which involves the successive chlorination and nitration salicylaldehyde (1) to 5-chloro-3-nitrosalicyladehyde (3). The coumarin was synthesized by using Perkin reaction of 5-chloro-3-nitrosalicyladehyde. The nitro coumarin (4) obtained was reduced to 8-amino-6-chloro coumarin (5) which was then treated with bromine and potassium thiocyanate followed by the treatment of ammonia gives 2-amino-4-chloro-8H-chromeno-[8,7-d]-1,3-thiazol-8-one (6). The final 2-aminobenzo-1,3-thiazole derivative was diazotized and coupled with different phenols and anilines to yield diazo compounds. These compounds are then subjected to biological characterization

A Promising Review on Cyclodextrin Conjugated Paclitaxel Nanoparticles for Cancer Treatment

This review presented the unique characteristics of different types of cyclodextrin polymers by non-covalent host&ndash;guest interactions to synthesize an inclusion complex. Various cancers are treated with different types of modified cyclodextrins, along with the anticancer drug paclitaxel. PTX acts as a mitotic inhibitor, but due to its low dissolution and permeability in aqueous solutions, it causes considerable challenges for drug delivery system (DDS) designs. To enhance the solubility, it is reformulated with derivatives of cyclodextrins using freeze-drying and co-solvent lyophilization methods. The present supramolecular assemblies involve cyclodextrin as a key mediator, which is encapsulated with paclitaxel and their controlled release at the targeted area is highlighted using different DDS. In addition, the application of cyclodextrins in cancer treatment, which reduces the off-target effects, is briefly demonstrated using various types of cancer cell lines. A new nano-formulation of PTX is used to improve the antitumor activity compared to normal PTX DDS in lungs and breast cancer is well defined in the present review